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RAFV600E和C-RAF-1抑制剂(VEMURAFENIB)

Vemurafenib

CAS: 1029872-54-5;918504-65-1

Molecular Formula: C23H18ClF2N3O3S

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RAFV600E和C-RAF-1抑制剂(VEMURAFENIB) - Names and Identifiers

Name Vemurafenib
Synonyms RG 7204
PLX 4032
RG 7204
RO 5185426
vemurafenib
Vemurafenib
RO 5185426
Plx-4032 (RG7024)
VeMurafenib,PLX 4032
N-(3-(5-(4-Chlorophenyl)-1H-pyrrolo[2,3-B]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonaMide
N-[3-[[5-(4-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-PropanesulfonaMide
N-(3-{[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl}-2,4-difluorophenyl)propane-1-sulfonaMide
N-[3-[[5-(4-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide
CAS 1029872-54-5
918504-65-1
EINECS 800-227-2

RAFV600E和C-RAF-1抑制剂(VEMURAFENIB) - Physico-chemical Properties

Molecular FormulaC23H18ClF2N3O3S
Molar Mass489.9221264
Density1.46
Melting Point>263oC (dec.)
Solubility Soluble in DMSO (100 mg/mL), and methanol. Insoluble in ethanol, and water
AppearanceSolid
ColorOff-White
Storage ConditionRefrigerator
UseA novel and potent inhibitor of B- RAFV600E with IC50 of 31 nM.

RAFV600E和C-RAF-1抑制剂(VEMURAFENIB) - Reference

Reference
Show more
1. [IF=9.162] Kun Zhao et al."Morusin enhances the antitumor activity of MAPK pathway inhibitors in BRAF-mutant melanoma by inhibiting the feedback activation of STAT3."Eur J Cancer. 2022 Apr;165:58

RAFV600E和C-RAF-1抑制剂(VEMURAFENIB) - Introduction

Vemurafenib (PLX4032, RG7204) is a new and effective B- Raf V600E inhibitor with IC50 of 31 nM.
Last Update:2022-10-16 17:11:36

RAFV600E和C-RAF-1抑制剂(VEMURAFENIB) - Reference Information

overview vilafenib (Vemurafenib), trade name Zelboraf, is a kinase inhibitor developed by Roche (HoffmannLaRoche) company for the treatment of patients with unresectable or metastatic melanoma and BRAFV600E mutations approved by FDA. it was approved by FDA in August 2011 for the treatment of advanced metastatic or unresectable melanoma.
Application Verofenib is a small molecule BRAF kinase inhibitor that can selectively bind to the ATP binding domain of mutant BRAF, thereby inhibiting the activation of the enzyme. The US Food and Drug Administration (FDA) has approved Verofenib for the treatment of malignant melanoma with BRAF gene mutation.
preparation preparation of vilafenib (I): add 250g of toluene and 31.5g (0.10 mol) N-[2] to a 500 ml four-mouth flask connected with stirring, thermometer and reflux condenser tube with water separator, 4-Difluoro-3-(cyanopropionyl) phenyl] n-propyl sulfonamide, 17.0 grams (0.11 moles) of p-chlorophenyl acetaldehyde, 0.5 grams of piperidine, heating, stirring, 83-85 ℃ azeotropic reflux with water Condensation reaction for 5 hours; cooling to 30 ℃, adding 38.0 grams (0.32 moles) of N,N-dimethylformamide dimethanol, stirring at 85-90 ℃ for 6 hours; cooling to 30 ℃, 70.0g of 10wt% ammonia methanol solution was added and stirred at 50~55 ℃ for 4 hours. Decompression distillation recovers methanol and toluene, adds 200 grams of isopropanol to the residue, heats to 80 ℃, cools, recrystallizes, filters, dries to obtain 43.9 kverafenib with 89.6% yield and 99.91% liquid phase purity.
Last Update:2024-04-09 21:11:58
RAFV600E和C-RAF-1抑制剂(VEMURAFENIB)
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CAS: 918504-65-1
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     tech@medchemexpress.com
Mobile: 609-228-6898
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Multiple SpecificationsSpot supply
Product Name: Plx-4032 Visit Supplier Webpage Request for quotation
CAS: 1029872-54-5
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Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
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Shanghai Macklin Biochemical Co., Ltd
Spot supply
Product Name: Vemurafenib (PLX4032, RG7204) Visit Supplier Webpage Request for quotation
CAS: 918504-65-1
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Yuanye Bio-Technology Co., Ltd.
Multiple SpecificationsSpot supply
Product Name: Vemurafenib (PLX4032, RG7204) Visit Supplier Webpage Request for quotation
CAS: 918504-65-1
Tel: 18301782025
Email: 3008007409@qq.com
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View History
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